Focused Sets: Wnt/ ß-catenin pathway inhibitors/activators

The Wnt/β-catenin signaling pathway plays a critical role in a broad range of biological systems including stem cell biology, developmental biology, and adult organ systems. Deregulation of the functional components of the pathway has been implicated in a wide spectrum of diseases including cancer, neuronal, skin, and cardiovascular disorders. Several components of Wnt/β-catenin signaling pathway represent valuable targets for drug discovery efforts.

Based on the structural analysis of known Wnt signaling modulators  we have crafted a library of small molecule compounds that can be exploited for discovery of novel chemical regulators of this pathway. The library comprises multiple chemotypes including various conformationally constrained compounds which mimic the a-helix secondary structure of peptides and proteins. This strategy was shown to be effective in delivering effective inhibitors of Wnt signaling by controlling the gene transcription or protein-protein interaction modulation mechanisms [1].

1. Alpha helix mimetic compositions for treating cancer and other cbp/catenin-mediated diseases and condition. Hiroyuki Kouji, Yuji Kogami, Takenao Odagami. US 20140221657 A1

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